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Assay Detail

CHEMBL4767577

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Binding
Inhibition of mouse GTA4 receptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

GABA transporter 4 (CHEMBL3699)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Novel mouse GABA uptake inhibitors with enhanced inhibitory activity toward mGAT3/4 and their effect on pain threshold in mice.
Zaręba P,Gryzło B,Malawska K,Sałat K,Höfner GC,Nowaczyk A,Fijałkowski Ł,Rapacz A,Podkowa A,Furgała A,Żmudzki P,Wanner KT,Malawska B,Kulig K
Eur J Med Chem (2020) 188 : 111920 -111920
PubMed 31901745 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.24 5.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4779064 1 5.78
CHEMBL419823 1 5.71
CHEMBL4566905 1 5.20
CHEMBL3289575 1 5.04
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 1 4.48
CHEMBL297569 BETA-ALANINE 1 -
CHEMBL4793097 1 -
CHEMBL4789121 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4779064 IC50 = 1659.59 nM 5.78
CHEMBL419823 IC50 = 1949.84 nM 5.71
CHEMBL4566905 IC50 = 6309.57 nM 5.20
CHEMBL3289575 IC50 = 9120.11 nM 5.04
CHEMBL96 GAMMA-AMINOBUTYRIC ACID IC50 = 33113.11 nM 4.48
CHEMBL297569 BETA-ALANINE IC50 = 109647.82 nM -
CHEMBL4793097 IC50 = 301995.17 nM -
CHEMBL4789121 IC50 = 301995.17 nM -